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化学学报
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化学学报 ›› 2006, Vol. 64 ›› Issue (18): 1911-1915. 上一篇    下一篇

研究论文

嘧啶并呋咱核苷衍生物的制备及其活性初探

邓艳君1, 石静波1, 姜力勋1, 高静2, 姚其正*,1   

  1. (1中国药科大学药学院 南京 210009)
    (2南京大学医学院 南京 210093)
  • 投稿日期:2005-12-09 修回日期:2006-01-23 发布日期:2006-09-28
  • 通讯作者: 姚其正

Synthesis of Pyrimidofuroxan-Nucleoside Derivatives and Preliminary Study of Their Activities

DENG Yan-Jun1; SHI Jing-Bo1; JIANG Li-Xun1; GAO Jing2; YAO Qi-Zheng*,1   

  1. (1 School of Pharmacy, China Pharmaceutical University, Nanjing 210009)
    (2 Medical School, Nanjing University, Nanjing 210093)
  • Received:2005-12-09 Revised:2006-01-23 Published:2006-09-28
  • Contact: YAO Qi-Zheng

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939

被引次数

33 | 6

4H,6H-[1,2,5]噁二唑并[3,4-d]嘧啶-5,7-二酮1-氧化物(1)和6-甲基-4H,6H-[1,2,5]噁二唑并[3,4-d]嘧啶-5,7-二酮1-氧化物(2)是一氧化氮(NO)供体, 将它们分别在无溶剂条件下与高温熔融的全乙酰基保护的核糖、木糖、葡萄糖进行糖基化反应, 分别得到相应的噁二唑并[3, 4-d]嘧啶核苷类化合物7, 9～12, 化合物7经NH3-MeOH处理, 去O-乙酰基制得8, 这些新型核苷化合物可作为潜在的NO供体. 部分此类化合物的生物活性研究表明, 嘧啶并呋咱核苷衍生物具有抗病毒、抗肿瘤活性, 为研究抗病毒、抗肿瘤药物提供了新结构类型的候选化合物.

关键词: 噁二唑并[3,4-d]嘧啶核苷, 抗肿瘤, 抗病毒

4H,6H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide (1) and 6-methyl-4H,6H-[1,2,5]- oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide (2) are nitric oxide (NO) donors. Their glycosidation, with peracetyl ribofuranose, xylfuranose and glucopyranose respectively, under solvent-free and fusion reaction conditions gives corresponding oxadiazolo[3,4-d]pyrimidine nucleoside derivatives 7, 9～12. The O-acetyl groups in nucleoside 7 are removed by the use of methanolic ammonia to yield compound 8. These new nucleosides may be as potential NO donors. Initial bioactivity tests show that pyrimidofuroxan-nucleosides have antivirus and anticancer effects. The research results provide new candidate molecules for study of antivirus and anticancer drugs.

Key words: oxadiazolo[3,4-d]pyrimidine nucleoside, antivirus, anticancer